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Cyanines have been widely used as the photosensitizers (PSs) in the biomedical field, but controlling their molecular aggregates in nanoparticles (NPs) remains a major challenge. Moreover, the impact of aggregate behaviors of cyanines on the photosensitization is still unclear. Herein, the first anionic cyanine PSs based on a tricyanofuran end group have been designed by achieving supramolecular J-type aggregates in NPs via counterion engineering. Our results indicate that J-type aggregates in NPs can not only bring significantly red-shifted emission, negatively charged surface, and high photostability, but also enable a significant 5-fold increase in singlet oxygen generation efficiency compared to that in the nonaggregate state, providing strong experimental evidence for the superiority of J-aggregates in enhancing photosensitization. Thus, combined with the mitochondria-targeting ability, the J-type aggregate NPs show remarkable in vivo antitumor phototheranostic efficacy, making them have a potential for clinical use.
Li et al. (Mon,) studied this question.